GSK2795039

製品コードS8974 バッチS897401

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₃H₂₆N₆O₂S

分子量

450.56

CAS No.

1415925-18-6

Solubility (25°C)*

体外

DMSO

90 mg/mL (199.75 mM)

Ethanol

20 mg/mL (44.38 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

10.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2) with pIC50 of 6.57 for NOX2-mediated activation of HRP/Amplex Red. GSK2795039 inhibits reactive oxygen species (ROS) production, NADPH consumption and reduces apoptosis.
in vitro	GSK2795039 inhibits both the formation of ROS and the utilization of the enzyme substrates, NADPH and oxygen, in a variety of semirecombinant cell-free and cell-based NOX2 assays. GSK2795039 inhibits NOX2 in an NADPH competitive manner and is selective over other NOX isoforms, xanthine oxidase, and endothelial nitric oxide synthase enzymes.^[1]
in vivo	Following systemic administration in mice, GSK2795039 abolishes the production of ROS by activated NOX2 enzyme in a paw inflammation model. GSK2795039 shows activity in a murine model of acute pancreatitis, reducing the levels of serum amylase triggered by systemic injection of cerulein.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NOX isoform-specific cells, PBMCs, PMNs, HL60 cells
	濃度	3.16 nM, 10 nM, 31.6 nM, 100 nM, 316 nM, 1μM, 3.16 μM, 10 μM, 31.6 μM, 100μM
	反応時間	10 min, 20 min, 30 min, 40 min, 50 min, 60 min
	実験の流れ	For Amplex Red/HRP assay, cells are preincubated with the GSK2795039 for 10 min at room temperature in PerkinElmer black 96-well microplates at 50,000 cells per well, after which the reaction mixture is added to a final concentration of 25 μM of Amplex Red and 0.05 U/ml of HRP in HBSS. NOX enzymes are activated via 100 nM PMA (NOX1, NOX2), 1 μg/ml tetracycline for 24-h activation of inducible genes (NOX3, NOX4), and 1 μM Ca²⁺ ionophore ionomycin (NOX5).
動物実験	動物モデル	Male Sprague-Dawley (SD) rats, C57BL6/J mice, gp91^phox knockout mice
	投薬量	2–100 mg/kg
	投与方法	IP

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Stachydrine Hydrochloride Regulates the NOX2-ROS-Signaling Axis in Pressure-Overload-Induced Heart Failure [ Int J Mol Sci, 2023, 24(18)14369]	PubMed: 37762672
Stachydrine Hydrochloride Regulates the NOX2-ROS-Signaling Axis in Pressure-Overload-Induced Heart Failure [ Int J Mol Sci, 2023, 10.3390/ijms241814369]	PubMed: 37762672
Oxidative stress mediated by the TLR4/NOX2 signalling axis is involved in polystyrene microplastic-induced uterine fibrosis in mice [ Sci Total Environ, 2022, 838(Pt 2):155825]	PubMed: 35597360
Lipopolysaccharide induces placental mitochondrial dysfunction in murine and human systems by reducing MNRR1 levels via a TLR4-independent pathway [ iScience, 2022, 25(11):105342]	PubMed: 36339251

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。